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Items: 1 to 20 of 84


Design, synthesis and biological evaluation of novel TRβ selective agonists sustained by ADME-toxicity analysis.

Runfola M, Sestito S, Bellusci L, La Pietra V, D'Amore VM, Kowalik MA, Chiellini G, Gul S, Perra A, Columbano A, Marinelli L, Novellino E, Rapposelli S.

Eur J Med Chem. 2019 Dec 23;188:112006. doi: 10.1016/j.ejmech.2019.112006. [Epub ahead of print]


Dual PDK1/Aurora Kinase A Inhibitors Reduce Pancreatic Cancer Cell Proliferation and Colony Formation.

Casari I, Domenichini A, Sestito S, Capone E, Sala G, Rapposelli S, Falasca M.

Cancers (Basel). 2019 Oct 31;11(11). pii: E1695. doi: 10.3390/cancers11111695.


Design and synthesis of H2S-donor hybrids: A new treatment for Alzheimer's disease?

Sestito S, Pruccoli L, Runfola M, Citi V, Martelli A, Saccomanni G, Calderone V, Tarozzi A, Rapposelli S.

Eur J Med Chem. 2019 Dec 15;184:111745. doi: 10.1016/j.ejmech.2019.111745. Epub 2019 Sep 27.


Lipolytic Effects of 3-Iodothyronamine (T1AM) and a Novel Thyronamine-Like Analog SG-2 through the AMPK Pathway.

Rogowski M, Bellusci L, Sabatini M, Rapposelli S, Rahman SM, Chiellini G, Assadi-Porter FM.

Int J Mol Sci. 2019 Aug 20;20(16). pii: E4054. doi: 10.3390/ijms20164054.


Preclinical validation of 3-phosphoinositide-dependent protein kinase 1 inhibition in pancreatic cancer.

Emmanouilidi A, Fyffe CA, Ferro R, Edling CE, Capone E, Sestito S, Rapposelli S, Lattanzio R, Iacobelli S, Sala G, Maffucci T, Falasca M.

J Exp Clin Cancer Res. 2019 May 14;38(1):191. doi: 10.1186/s13046-019-1191-2.


Multi-targeted ChEI-copper chelating molecules as neuroprotective agents.

Sestito S, Wang S, Chen Q, Lu J, Bertini S, Pomelli C, Chiellini G, He X, Pi R, Rapposelli S.

Eur J Med Chem. 2019 Jul 15;174:216-225. doi: 10.1016/j.ejmech.2019.04.060. Epub 2019 Apr 23.


A patent update on PDK1 inhibitors (2015-present).

Sestito S, Rapposelli S.

Expert Opin Ther Pat. 2019 Apr;29(4):271-282. doi: 10.1080/13543776.2019.1597852. Epub 2019 Mar 29. Review.


Memantine prodrug as a new agent for Alzheimer's Disease.

Sestito S, Daniele S, Pietrobono D, Citi V, Bellusci L, Chiellini G, Calderone V, Martini C, Rapposelli S.

Sci Rep. 2019 Mar 15;9(1):4612. doi: 10.1038/s41598-019-40925-8.


Editorial: Multi-Target-Directed Ligands (MTDL) as Challenging Research Tools in Drug Discovery: From Design to Pharmacological Evaluation.

Alcaro S, Bolognesi ML, García-Sosa AT, Rapposelli S.

Front Chem. 2019 Feb 18;7:71. doi: 10.3389/fchem.2019.00071. eCollection 2019. No abstract available.


Epibatidine: A Promising Natural Alkaloid in Health.

Salehi B, Sestito S, Rapposelli S, Peron G, Calina D, Sharifi-Rad M, Sharopov F, Martins N, Sharifi-Rad J.

Biomolecules. 2018 Dec 23;9(1). pii: E6. doi: 10.3390/biom9010006. Review.


New Multitarget Approaches in the War Against Glioblastoma: A Mini-Perspective.

Sestito S, Runfola M, Tonelli M, Chiellini G, Rapposelli S.

Front Pharmacol. 2018 Aug 3;9:874. doi: 10.3389/fphar.2018.00874. eCollection 2018.


New Insights into the Potential Roles of 3-Iodothyronamine (T1AM) and Newly Developed Thyronamine-Like TAAR1 Agonists in Neuroprotection.

Bellusci L, Laurino A, Sabatini M, Sestito S, Lenzi P, Raimondi L, Rapposelli S, Biagioni F, Fornai F, Salvetti A, Rossi L, Zucchi R, Chiellini G.

Front Pharmacol. 2017 Dec 12;8:905. doi: 10.3389/fphar.2017.00905. eCollection 2017.


A review on the hybrids of hydroxycinnamic acid as multi-target-directed ligands against Alzheimer's disease.

Zhang X, He X, Chen Q, Lu J, Rapposelli S, Pi R.

Bioorg Med Chem. 2018 Feb 1;26(3):543-550. doi: 10.1016/j.bmc.2017.12.042. Epub 2017 Dec 26. Review.


Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.

Nesi G, Chen Q, Sestito S, Digiacomo M, Yang X, Wang S, Pi R, Rapposelli S.

Eur J Med Chem. 2017 Dec 1;141:232-239. doi: 10.1016/j.ejmech.2017.10.006. Epub 2017 Oct 4.


Hydrogen Sulfide: A Worthwhile Tool in the Design of New Multitarget Drugs.

Sestito S, Nesi G, Pi R, Macchia M, Rapposelli S.

Front Chem. 2017 Sep 27;5:72. doi: 10.3389/fchem.2017.00072. eCollection 2017.


Sulfonamido-derivatives of unsubstituted carbazoles as BACE1 inhibitors.

Bertini S, Ghilardi E, Asso V, Minutolo F, Rapposelli S, Digiacomo M, Saccomanni G, Salmaso V, Sturlese M, Moro S, Macchia M, Manera C.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4812-4816. doi: 10.1016/j.bmcl.2017.09.058. Epub 2017 Sep 28.


A Novel H2S-releasing Amino-Bisphosphonate which combines bone anti-catabolic and anabolic functions.

Rapposelli S, Gambari L, Digiacomo M, Citi V, Lisignoli G, Manferdini C, Calderone V, Grassi F.

Sci Rep. 2017 Sep 20;7(1):11940. doi: 10.1038/s41598-017-11608-z.


Iminothioethers as Hydrogen Sulfide Donors: From the Gasotransmitter Release to the Vascular Effects.

Barresi E, Nesi G, Citi V, Piragine E, Piano I, Taliani S, Da Settimo F, Rapposelli S, Testai L, Breschi MC, Gargini C, Calderone V, Martelli A.

J Med Chem. 2017 Sep 14;60(17):7512-7523. doi: 10.1021/acs.jmedchem.7b00888. Epub 2017 Aug 25.


Oxidative Stress, Mitochondrial Abnormalities and Proteins Deposition: Multitarget Approaches in Alzheimer's Disease.

Nesi G, Sestito S, Digiacomo M, Rapposelli S.

Curr Top Med Chem. 2017;17(27):3062-3079. doi: 10.2174/1568026617666170607114232. Review.


Synthesis and Functional Evaluation of Novel Aldose Reductase Inhibitors Bearing a Spirobenzopyran Scaffold.

Digiacomo M, Sartini S, Nesi G, Sestito S, Coviello V, La Motta C, Rapposelli S.

Open Med Chem J. 2017 Jan 31;11:9-23. doi: 10.2174/1874104501711010009. eCollection 2017.

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